GI254023X

GI254023X is a **small molecule inhibitor** that selectively inhibits the metalloproteinases ADAM10 (IC50 5.3 nM) and MMP9 (IC50 2.5 nM)[1][9][11]. GI254023X acts as a zinc-binding hydroxamate, chelating the zinc at the protease active site to inhibit ADAM10 activity[4][5][10]. It is used primarily as a research tool for investigating the role of ADAM10 in neurodegeneration, inflammation, cancer, and traumatic brain injury (TBI)[2][7][10]. Pharmacologically, GI254023X has shown neuroprotective effects in animal models, reducing brain tissue loss, axonal injury, and proinflammatory cytokine expression following TBI[2]. It also inhibits cell migration and invasion by targeting ADAM10 and MMP9 activity[1][4]. Development as a clinical drug was terminated in Phase 1/2 due to hepatotoxicity[4].

Brand names

GI254023XGI-254023XGI 254023X

Other names

GI254023XGI-254023XGI 254023XGI4023GI-4023GI 4023